针对磺酰脲类（ALS酶）除草剂在轮作农田中对后茬敏感作物造成严重药害,申请者以前期研究发现的活性模板结构dichloroacetyloxazol先导物具有较好的安全剂活性，并建立了构效关系模型。在此基础上，以苯并含氮杂环为母体，采用活性亚结构拼接的方式，运用生物合理设计、合成系列新型卤代磺酰取代芳（氧）氮杂桥环类结构，采用生物测定的方法研究新结构对保护作物的酶活性、作物的抗逆性及除草剂作用的生理过程的影响，确定作用于ALS靶标点的化合物骨架结构特征，建立安全剂结构与活性的构效关系，筛选出具有高活性的1-2个磺酰脲类除草剂的安全剂结构，并根据模型结果指导合成高活性磺酰氧（氮）杂桥环类安全剂。本研究对于创制具有自主知识产权的新型磺酰脲类除草剂的安全剂具有重要的理论和实际意义，又为新安全剂结构优化和研发提供科学依据。

The acetolactate synthase(ALS)inhibitors caused serious injury to the following sensitive crops in the rotation fields. With the dichloroacetyloxazol as the leader compound, we design and synthesis of the novel substituted halide sulfonyl aromatic aza heterocycles and substituted halide sulfonyl oxa aza heterocycles according to the structure activity related theory and bio-rational design. It will be probed that the effects of the novel compounds on enzymes activity and herbicide metabolism physical processes in the crops. The skeleton characteristic is defined and the QSAR (quantitative structure activity relationships) models are also constructed. The main object of this project is to obtain 1-2 novel ALS inhibitors safeners with high herbicidal activity to apply the patent. The results of this study could provide the technology to apply the old herbicides in safe way; enlarge the application area of old herbicides; solve the ALS inhibitors phytotoxicity, and probe a new method to design and develop novel herbicide safeners.